Table 5.
Antiviral activity against herpes virus-1 (HSV-1), herpes virus-2 (HSV-2), acyclovir-resistant HSV (Thymidine kinase knock-out) and vaccinia virus cultured in Hel (human embryonic lung) cells.
| Cpd | HSV-1 (KOS) EC50a (μM) | HSV-2 (G) EC50a (μM) | HSV-1 (TK−) KOS ACVr EC50a (μM) | vaccinia virus EC50a (μM) | MCCb (μM) | CC50c (μM) |
|---|---|---|---|---|---|---|
| 5 | >4 | >4 | >4 | 0.35 ± 0.05 | 20 | 0.73 ± 0.07 |
| 59 | 2.10 ± 0.97 | 0.63 ± 0.09 | 1.27 ± 0.52 | 0.73 ± 0.33 | ≥20 | N.D. |
| 66 | 16.3 ± 3.7 | >100 | 10.57 ± 4.84 | >100 | ≥100 | 5.25 ± 3.80 |
| 67 | 6.67 ± 2.67 | >100 | 5.83 ± 3.17 | >100 | >100 | 0.35 ± 0.02 |
| 68 | >100 | >100 | >100 | >100 | >100 | 0.16 ± 0.0 |
| 70 | >100 | >100 | >100 | >100 | >100 | N.D. |
| Acyclovir | 0.2 | 0.2 | 10 | >250 | >250 | N.D. |
| Cidofovir | 1.5 | 1.2 | 2.0 | 22 | >250 | N.D. |
| Ganciclovir | 0.03 | 0.03 | 0.5 | >100 | >100 | N.D. |
a
Antiviral activity is expressed as EC50 values (μM) and represent the concentration of test compound necessary to reduce viral-induced cytopathogenicity by 50%.
b
MCC or minimal cytotoxic concentration represents the concentration of test compound that is able to cause a microscopically detectable alteration of normal cell morphology.
c
CC50 represents the concentration (μM) of test compound that reduces cell (Hel) proliferation by 50% as determined by Coulter Counter.